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12 条记录 (耗时 0.015 秒)

    THYROID FUNCTION IMPROVER
    1.
    发明专利
    THYROID FUNCTION IMPROVER 失效

    公开(公告)号：JPH0616554A

    公开(公告)日：1994-01-25

    申请号：JP17395292

    申请日：1992-07-01

    申请人： ASAHI CHEMICAL IND

    发明人： KAWAKUBO HIROSHI ,  HASE TADASHI ,  ENDOU TOYOSHI

    IPC分类号： A61K31/435 ,  A61P5/12 ,  A61P43/00 ,  C07D491/048 ,  C07D495/04

    摘要： PURPOSE:To obtain a thyroid function improver for preventing and improving functional disorder of thyroid tissue and symptoms and sequela caused by the disorder, comprising a benzothienopyridine as an active ingredient. CONSTITUTION:The thyroid function improver comprises a compound of formula I of formula II (R1 is alkoxy, amino, hydrazino or N-containing heterocyclic group; R2 and R3 are halogen, alkyl, aryl, alkenyl, acyl, etc.; m and n are 0-4; etc.) such as benzo[b]thieno[2, 3-c]pyridine-3-carboxylic acid methyl ester as an active ingredient. In the case of pharmaceutical manufacturing of the compound into capsule, tablet, granule or powder form, 1-80wt.% of the compound is contained, in the case of to injection, 0.01-20wt.% of the compound is contained and in the case of into syrup and suspension is 0.01-20wt.% of the compound is contained. The improver is effective against thyroidism, Basedow's disease, Plummer's disease, cretin disease, insanity and intelectural disturbance caused by hypothyroidism, Paget's disease, osteoporosis, etc.

    TETRAHYDROPYRIDINE DERIVATIVE HAVING SUBSTITUENT ON THREE RINGS
    3.
    发明专利
    TETRAHYDROPYRIDINE DERIVATIVE HAVING SUBSTITUENT ON THREE RINGS 失效

    公开(公告)号：JPH05163278A

    公开(公告)日：1993-06-29

    申请号：JP12670692

    申请日：1992-04-21

    申请人： ASAHI CHEMICAL IND

    发明人： KAWAKUBO HIROSHI ,  HASE TADASHI ,  UEKI AKIKAZU

    IPC分类号： A61K31/435 ,  A61P25/00 ,  A61P25/20 ,  A61P25/28 ,  C07D495/04

    摘要： PURPOSE:To provide a new compound having low toxicity and useful as an antianxiety agent and a learning ability improving agent. CONSTITUTION:The compound of formula I (A is S, sulfoxido or sulfone; R1 is 4-hydroxycyclohexylamino, 4-methylcyclohexylamino, etc.; R2 and R3 are H or hydroxy; (m) and (n) are 0-4; when (m) and (n) are >=2, plural R2 or R3 may be the same or different), e.g. N-(trans-4-hydroxycyclohexyl)-1,2,3,4- tetrahydro-benzo [b]thieno [2,3-C]pyridine-3-carbamide. The compound of formula I can be produced e.g. by preparing a compound of formula III from a compound of formula II used as a starting raw material and deprotecting the compound of formula III in an acidic solvent such as acetic acid.

    CEREBRAL FUNCTION-IMPROVING AGENT
    4.
    发明专利
    CEREBRAL FUNCTION-IMPROVING AGENT 失效

    公开(公告)号：JPH04173735A

    公开(公告)日：1992-06-22

    申请号：JP29883590

    申请日：1990-11-06

    申请人： ASAHI CHEMICAL IND

    发明人： KAWAKUBO HIROSHI ,  HASE TADASHI

    IPC分类号： C07D491/048 ,  A61K31/435 ,  A61P25/18 ,  A61P25/28 ,  C07D495/04

    摘要： PURPOSE:To provide a cerebral function-improving agent containing a tetrahydropyridine derivative or an acid adduct thereof as an active ingredient and not causing an anesthetic state, disorders accompanied thereby, etc. CONSTITUTION:A cerebral function-improving agent contains a compound of the formula (A is S, O; R1 is alkoxy, amino, ureido, N-containing 6 or 7-membered heterocyclic group; R2, R3 are halogen, alkyl, aryl, alkenyl, acyl, arylcarbonyl; (m), (n) are 0-4) or an acid adduct thereof, such as N- cyclohexyl-1,2,3,4-tetrahydrobenzo[b]thieno[2,3-c]pyridine-3-carboxamide hydrochloride as an active ingredient. The compound has effects of maintaining, improving and stimulating on cerebral metabolism, a cerebral cell and function- protecting activity, and a cerebral infarctional nest formation-inhibiting activity, and is administered in a dose of 0.01-20mg/kg.day in parenteral administration and in a dose of 0.02-40mg/kg.day in oral administration.

    PYRIDINE DERIVATIVE
    5.
    发明专利
    PYRIDINE DERIVATIVE 失效

    公开(公告)号：JPH01100172A

    公开(公告)日：1989-04-18

    申请号：JP25471287

    申请日：1987-10-12

    申请人： ASAHI CHEMICAL IND

    发明人： UEKI AKIKAZU ,  KAWAKUBO HIROSHI ,  OKAZAKI KATSUYA ,  HASE TADASHI

    IPC分类号： A61K31/435 ,  A61P25/20 ,  A61P25/28 ,  C07D491/048 ,  C07D495/04

    摘要： NEW MATERIAL:A compound formula I [A is S or O; R1 is (substituted)amino, hydrazino or 6- or 7-membered heterocyclic group containing one or more N atoms; R2 and R3 are halogen, (substituted)alkyl or aryl; m is 0-2; n is 0-4] and salts thereof. EXAMPLE:N-(2-Aminoethyl)-benzo[b]thieno[2,3-c]pyridine-3-carboamide hydrochloride. USE:A medicine and psychotropic agent having antianxiety and learning improving action. PREPARATION:For example, a compound expressed by formula II is reacted with a compound expressed by formula VIII (R4 is H or R2) to form a compound expressed by formula III, which is then reacted with a compound expressed by formula IX to afford a compound expressed by formula IV. The resultant compound expressed by formula IV is subsequently reacted with Fe and HCl to form a compound expressed by formula V, which is then reacted with a compound expressed by formula X (R4' is same as R4) to provide a compound expressed by formula VI. The obtained compound expressed by formula VI is subsequently reacted with a compound expressed by the formula HX1 (X1 is leaving group, etc.) and then dehydrosulfurized with NaHCO3 and S to provide the aimed compound expressed by formula I.

    TETRAHYDROPYRIDINE DERIVATIVE HAVING HYDROPHOBIC SUBSTITUENT GROUP ON THIRD RING
    6.
    发明专利
    TETRAHYDROPYRIDINE DERIVATIVE HAVING HYDROPHOBIC SUBSTITUENT GROUP ON THIRD RING 失效

    公开(公告)号：JPH0853458A

    公开(公告)日：1996-02-27

    申请号：JP22272995

    申请日：1995-08-09

    申请人： ASAHI CHEMICAL IND

    发明人： KAWAKUBO HIROSHI ,  HASE TADASHI ,  UEKI AKIKAZU

    IPC分类号： C07D495/04 ,  A61K31/435 ,  A61K31/44 ,  A61K31/445 ,  A61K31/495 ,  A61P25/00 ,  A61P25/20 ,  A61P25/28

    摘要： PURPOSE:To provide a new compound having an anxiolytic effect and a learning-improving effect and useful as a low-toxic psychotropic agent. CONSTITUTION:This compound is expressed by formula I [R is 4-(or 2) hydroxycyclohexylamino, 4-(or 2)methylcyclohexylamino, 4-tert- butylcyclohexylamino, 4-aminocyclohexylamino, piperidinoamino, etc.], e.g. N-(2-hydroxy-cyclohexyl)-1,2,3,4-tetrahydrobenzo[b]thieno[2,4-C]pyridi ne-3- carbamide. The compound of formula I is synthesized by reacting the compound of formula II (BOC is tertiary butoxycarbonyl) with a compound of the formula RH in the presence of a condensation agent (e.g. DCC) in a solvent (e.g. DMF) at 10 to 100 deg.C for 1 to 10hr. This compound is administrated in an amount of 0.01 to 20mg/kg/day or 0.02 to 40mg/kg/day respectively in the case of parenteral administration or oral administration.

    THERAPEUTIC AGENT FOR DEPRESSION
    7.
    发明专利
    THERAPEUTIC AGENT FOR DEPRESSION 失效

    公开(公告)号：JPH06263638A

    公开(公告)日：1994-09-20

    申请号：JP5230793

    申请日：1993-03-12

    申请人： ASAHI CHEMICAL IND

    发明人： KITAMURA YOSHIHISA ,  HASE TADASHI ,  MOCHIZUKI DAISUKE

    IPC分类号： A61K31/495 ,  A61P25/24 ,  A61P25/26 ,  C07D295/02

    摘要： PURPOSE:To obtain a therapeutic agent for depression having high safety, comprising 1-(2,3-dimethylphenyl)piperazine having excellent antidepressive effect or its acid addition salt as active ingredients. CONSTITUTION:A new therapeutic agent for depression comprises 1-(2,3- dimethylphenyl)piperazine of the formula or its acid addition salt as an active ingredient and has an action mechanism different from that of a conventional therapeutic agent. Hydrobromic acid, sulfuric acid, acetic acid, citric acid, benzoic acid, aspartic acid, etc., may be cited as the acid of the acid addition salt. This therapeutic agent of depression is promising to prevent and improve depression, a depressive state and body symptoms followed by them or to alleviate progress of the disorder. The therapeutic agent for depression is useful as a therapeutic agent for serious depression, depressive feeling, bipolar disorder, anxiety disorder, expression disorder of body, dissociated disorder, sexual disorder, sleep disorder, falsification disorder, adjustment disorder, personality disorder and body symptoms caused by the diseases such as gastric ulcer, duodenal ulcer, ulcerative colitis and hypersensitive colitis.

    TETRAHYDROPYRIDINE DERIVATIVE
    9.
    发明专利
    TETRAHYDROPYRIDINE DERIVATIVE 失效

    公开(公告)号：JPH02149583A

    公开(公告)日：1990-06-08

    申请号：JP25709588

    申请日：1988-10-14

    申请人： ASAHI CHEMICAL IND

    发明人： UEKI AKIKAZU ,  KAWAKUBO HIROSHI ,  OKAZAKI KATSUYA ,  HASE TADASHI

    IPC分类号： C07D491/048 ,  A61K31/435 ,  A61K31/505 ,  A61K31/535 ,  A61K31/55 ,  A61P25/18 ,  A61P25/20 ,  A61P25/28 ,  C07D495/04

    摘要： NEW MATERIAL:The compound of formula I [A is S or O; R1 is (substituted) alkoxy, amino, etc.; R2 and R3 are halogen, acyl, etc.; m and n are 0-4] and its salt. EXAMPLE:1,2,3,4-Tetrahydro-benzo[b]thieno[2,3-C]pyridine-3-carboxylic acid ethyl ester. USE:Psychotropic agent. The compound has antianxiety effect and learning- improving effect. PREPARATION:The objective compound is produced by (1) reacting a compound of formula 11 with a compound of formula III (R4 is H or R2), (2) reacting the resultant compound of formula IV with a compound of formula NO2 CH2COR1 to obtain a compound of formula V, (3) reacting the compound with HCl in the presence of iron powder, (4) reacting the obtained compound of formula VI with an aldehyde of formula R'4CHO (R'4 is R4) to produce a compound of formula VII, (5) reacting the product with a compound of formula HX1 (X1 is halogen, etc.) and finally (6) reacting the obtained compound of formula VIII with a base and a compound of formula R''4X2 (R''4 is R2; X2 is X1).

    NOVEL CYCLIC AMIDE COMPOUND
    10.
    发明专利
    NOVEL CYCLIC AMIDE COMPOUND 失效

    公开(公告)号：JPS6396189A

    公开(公告)日：1988-04-27

    申请号：JP24216486

    申请日：1986-10-14

    申请人： ASAHI CHEMICAL IND

    发明人： KAWAKUBO HIROSHI ,  OKAZAKI KATSUYA ,  HASE TADASHI ,  UEKI AKIKAZU

    IPC分类号： C07D495/04 ,  A61K31/435 ,  A61P21/02 ,  A61P25/00 ,  A61P25/08 ,  A61P25/20 ,  C07D491/048

    摘要： NEW MATERIAL:The compound of formula I [A is S or O; R is group of formula II (B is ethylene, trimethylene, etc.; C is ethylene, etc.; Z is methylene, N, O, S, etc.)] and its salt. EXAMPLE:1-(Benzo[b]thieno[2.3-C]pyridine-3-carbonyl)-piperidine. USE:Antianxiety agent and antidemential agent. PREPARATION:The compound of formula I can be produced e.g. by (1) reacting the compound of formula II (e.g. 3-chloromethylbenzothiopene) with acetaminomalonic acid diethyl ester, (2) hydrolyzing the reaction product, (3) heating the hydrolyzed compound in the presence of an alkali, (4) esterifying the resultant alpha-amino acid of formula III, (5) thermally cyclizing the ester in the presence of formaldehyde, (6) hydrolyzing to the carboxylic acid compound of formula IV and finally (7) reacting the compound with the compound of formula HR (e.g. piperidine).